Canagliflozin

Identification

Summary

Canagliflozin is a sodium-glucose co-transporter 2 (SGLT2) inhibitor used to manage hyperglycemia in type 2 diabetes mellitus (DM). Also used to reduce the risk of major cardiovascular events in patients with established cardiovascular disease and type 2 DM.

Brand Names
Invokamet, Invokana
Generic Name
Canagliflozin
DrugBank Accession Number
DB08907
Background

Canagliflozin, also known as Invokana, is a sodium-glucose cotransporter 2 (SGLT2) inhibitor used in the management of type 2 diabetes mellitus along with lifestyle changes including diet and exercise Label.

It was initially approved by the FDA in 2013 for the management of diabetes and later approved in 2018 for a second indication of reducing the risk of cardiovascular events in patients diagnosed with type 2 diabetes mellitus 8, Label.

Canagliflozin is the first oral antidiabetic drug approved for the prevention of cardiovascular events in patients with type 2 diabetes 8. Cardiovascular disease is the most common cause of death in these patients 4.

Type
Small Molecule
Groups
Approved
Structure
Weight
Average: 444.516
Monoisotopic: 444.140672805
Chemical Formula
C24H25FO5S
Synonyms
  • Canagliflozin
  • Canagliflozin anhydrous
  • Canagliflozina

Pharmacology

Indication

This drug is used in conjunction with diet and exercise to increase glycemic control in adults diagnosed with type 2 diabetes mellitus Label.

Another indication for canagliflozin is the prevention of major cardiovascular events (myocardial infarction, stroke, or death due to a cardiovascular cause) in patients with type 2 diabetes, as well as hospitalization for heart failure in patients with type 2 diabetes8,10.

In addition to the above, canagliflozin can be used to lower the risk of end-stage kidney disease and major increases in serum creatinine and cardiovascular death for patients with a combination of type 2 diabetes mellitus, diabetic nephropathy, and albuminuria.10

It is important to note that this drug is not indicated for the treatment of type 1 diabetes mellitus or diabetic ketoacidosis Label.

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Used in combination to preventCardiovascular mortalityCombination Product in combination with: Metformin (DB00331)••••••••••••••••••••••••• •••••••••••• •••• • •••••••• ••••••••• •••••••••••••••••
Prevention ofCardiovascular mortality••••••••••••••••••••••••••••• •••• • •••••••• ••••••••• •••••••• •••••••••••••••••
Used in combination to preventEnd stage renal disease (esrd)Combination Product in combination with: Metformin (DB00331)••••••••••••••••••••• • •••••••• ••••••••• •••••••• •••••••••••• •••••••••••••••••
Prevention ofEnd stage renal disease (esrd)••••••••••••••••••••• • •••••••• ••••••••• •••••••• •••••••••••• •••••••••••••••••
Used in combination to preventHospitalizationsCombination Product in combination with: Metformin (DB00331)••••••••••••••••••••••••• •••••••••••• •••••••••••• •••• • •••••••• ••••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

This drug increases urinary glucose excretion and decreases the renal threshold for glucose (RTG) in a dose-dependent manner Label. The renal threshold is defined as the lowest level of blood glucose associated with the appearance of detectable glucose in the urine 2,7. The end result of canagliflozin administration is increased urinary excretion of glucose and less renal absorption of glucose, decreasing glucose concentration in the blood and improving glycemic control.

A note on type 2 diabetes and cardiovascular disease

The risk of cardiovascular events in diabetes type 2 is increased due to the damaging effects of diabetes on blood vessels and nerves in the cardiovascular system. In particular, there is a tendency for hyperglycemia to create pro-atherogenic (plaque forming) lesions in blood vessels, leading to various fatal and non-fatal events including stroke and myocardial infarction 5,9. Long-term glycemic control has been proven to be effective in the prevention of cardiovascular events such as myocardial infarction and stroke in patients with type 2 diabetes 6.

Mechanism of action

The sodium-glucose co-transporter2 (SGLT2), is found in the proximal tubules of the kidney, and reabsorbs filtered glucose from the renal tubular lumen. Canagliflozin inhibits the SGLT2 co-transporter. This inhibition leads to lower reabsorption of filtered glucose into the body and decreases the renal threshold for glucose (RTG), leading to increased glucose excretion in the urine Label.

TargetActionsOrganism
ASodium/glucose cotransporter 2
inhibitor
Humans
Absorption

Bioavailability and steady-state

The absolute oral bioavailability of canagliflozin, on average, is approximately 65% Label. Steady-state concentrations are achieved after 4 to 5 days of daily dose administration between the range of 100mg to 300mg Label.

Effect of food on absorption

Co-administration of a high-fat meal with canagliflozin exerted no appreciable effect on the pharmacokinetic parameters of canagliflozin. This drug may be administered without regard to food. Despite this, because of the potential of canagliflozin to decrease postprandial plasma glucose excretion due to prolonged intestinal glucose absorption, it is advisable to take this drug before the first meal of the day Label.

Volume of distribution

This drug is extensively distributed throughout the body. On average, the volume of distribution of canagliflozin at steady state following a single intravenous dose in healthy patients was measured to be 83.5 L Label.

Protein binding

Canagliflozin is mainly bound to albumin. The plasma protein binding of this drug is 99% Label.

Metabolism

Canagliflozin is primarily metabolized by O-glucuronidation. It is mainly glucuronidated by UGT1A9 and UGT2B4 enzymes to two inactive O-glucuronide metabolites Label.

The oxidative metabolism of canagliflozin by hepatic cytochrome enzyme CYP3A4 is negligible (about 7%) in humans Label.

Hover over products below to view reaction partners

Route of elimination

After a single oral radiolabeled dose canagliflozin dose to healthy subjects, the following ratios of canagliflozin or metabolites were measured in the feces and urine Label:

Feces

41.5% as the unchanged radiolabeled drug

7.0% as a hydroxylated metabolite

3.2% as an O-glucuronide metabolite

Urine

About 33% of the ingested radiolabled dose was measured in the urine, generally in the form of O-glucuronide metabolites. Less than 1% of the dose was found excreted as unchanged drug in urine.

Half-life

In a clinical study, the terminal half-life of canagliflozin was 10.6 hours for the 100mg dose and 13.1 hours for the 300 mg dose Label.

Clearance

In healthy subjects, canagliflozin clearance was approximately 192 mL/min after intravenous (IV) administration Label.

The renal clearance of 100 mg and 300 mg doses of canagliflozin was measured to be in the range of 1.30 - 1.55 mL/min Label.

Adverse Effects
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Toxicity

Overdose information

If an overdose occurs, contact the Poison Control Center. Normal supportive measures should be taken, including the removal unabsorbed drug from the gastrointestinal tract, initiating clinical monitoring of the patient, and providing supportive treatment as deemed necessary. Canagliflozin has been removed in very small quantities after a 4-hour hemodialysis session. This drug is likely not dialyzable by peritoneal dialysis Label.

Pregnancy and lactation

Animal data has demonstrated that canagliflozin may cause adverse renal effects in a growing fetus. Data are insufficient at this time in determining a potential canagliflozin related risk for major birth defects or possible miscarriage in humans Label. There are known risks, however, of uncontrolled diabetes in pregnancy Label. Inform female patients taking canagliflozin of the potential risk, which is increased during the second and third trimesters. This drug is not recommended during nursing Label.

Mutagenesis and carcinogenicity

Canagliflozin was not found to be mutagenic in both metabolically activated and inactivated states in the Ames assay. Canagliflozin showed mutagenicity in laboratory mouse lymphoma assay, but only in the activated state. Canagliflozin was not found to be mutagenic in several in vivo assays performed on rats Label.

The carcinogenic risk of canagliflozin was assessed in 2-year studies completed in both CD1 mice and Sprague-Dawley rats. Canagliflozin was not shown to increase tumor incidence in mouse models given doses less than or equal to 14 times the exposure from a typical 300 mg dose in humans. Despite these negative findings in mice, the incidence of several tumors increased in mice, including Leydig cell tumors, renal tubular adenomas, and adrenal pheochromocytomas Label.

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbacavirAbacavir may decrease the excretion rate of Canagliflozin which could result in a higher serum level.
AbaloparatideThe risk or severity of adverse effects can be increased when Abaloparatide is combined with Canagliflozin.
AbametapirThe serum concentration of Canagliflozin can be increased when it is combined with Abametapir.
AbemaciclibThe serum concentration of Abemaciclib can be increased when it is combined with Canagliflozin.
AbrocitinibThe serum concentration of Canagliflozin can be increased when it is combined with Abrocitinib.
Food Interactions
  • Avoid alcohol. Excess alcohol intake may promote ketoacidosis.
  • Drink plenty of fluids.
  • Take before a meal. It is recommended to take this drug before the first meal of the day.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Canagliflozin hydrate0SAC974Z85928672-86-0VHOFTEAWFCUTOS-TUGBYPPCSA-N
Product Images
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
InvokanaTablet, film coated100 mgOralJanssen Cilag International Nv2020-12-16Not applicableEU flag
InvokanaTablet, film coated300 mg/1OralJanssen Pharmaceuticals, Inc.2013-03-29Not applicableUS flag
InvokanaTablet, film coated300 mgOralJanssen Cilag International Nv2020-12-16Not applicableEU flag
InvokanaTablet, film coated300 mg/1OralA-S Medication Solutions2013-03-29Not applicableUS flag
InvokanaTablet, film coated100 mgOralJanssen Cilag International Nv2020-12-16Not applicableEU flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
InvokametCanagliflozin hydrate (150 mg/1) + Metformin hydrochloride (1 g/1)Tablet, film coatedOralbryant ranch prepack2014-08-08Not applicableUS flag
InvokametCanagliflozin hydrate (150 mg/1) + Metformin hydrochloride (500 mg/1)Tablet, film coatedOralJanssen Pharmaceuticals, Inc.2014-08-08Not applicableUS flag
InvokametCanagliflozin (150 mg) + Metformin hydrochloride (1000 mg)TabletOralJanssen Pharmaceuticals2016-06-28Not applicableCanada flag
InvokametCanagliflozin (50 mg) + Metformin hydrochloride (500 mg)TabletOralJanssen Pharmaceuticals2016-06-28Not applicableCanada flag
InvokametCanagliflozin (150 mg) + Metformin hydrochloride (850 mg)TabletOralJanssen Pharmaceuticals2016-06-282022-09-06Canada flag

Categories

ATC Codes
A10BD16 — Metformin and canagliflozinA10BK02 — Canagliflozin
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as phenolic glycosides. These are organic compounds containing a phenolic structure attached to a glycosyl moiety. Some examples of phenolic structures include lignans, and flavonoids. Among the sugar units found in natural glycosides are D-glucose, L-Fructose, and L rhamnose.
Kingdom
Organic compounds
Super Class
Organic oxygen compounds
Class
Organooxygen compounds
Sub Class
Carbohydrates and carbohydrate conjugates
Direct Parent
Phenolic glycosides
Alternative Parents
Hexoses / C-glycosyl compounds / Toluenes / Fluorobenzenes / 2,5-disubstituted thiophenes / Oxanes / Aryl fluorides / Heteroaromatic compounds / Secondary alcohols / Polyols
show 5 more
Substituents
2,5-disubstituted thiophene / Alcohol / Aromatic heteromonocyclic compound / Aryl fluoride / Aryl halide / Benzenoid / C-glycosyl compound / Dialkyl ether / Ether / Fluorobenzene
show 17 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
organofluorine compound, thiophenes, ring assembly, C-glycosyl compound (CHEBI:73274)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
6S49DGR869
CAS number
842133-18-0
InChI Key
XTNGUQKDFGDXSJ-ZXGKGEBGSA-N
InChI
InChI=1S/C24H25FO5S/c1-13-2-3-15(24-23(29)22(28)21(27)19(12-26)30-24)10-16(13)11-18-8-9-20(31-18)14-4-6-17(25)7-5-14/h2-10,19,21-24,26-29H,11-12H2,1H3/t19-,21-,22+,23-,24+/m1/s1
IUPAC Name
(2S,3R,4R,5S,6R)-2-(3-{[5-(4-fluorophenyl)thiophen-2-yl]methyl}-4-methylphenyl)-6-(hydroxymethyl)oxane-3,4,5-triol
SMILES
[H][C@]1(O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)C1=CC=C(C)C(CC2=CC=C(S2)C2=CC=C(F)C=C2)=C1

References

General References
  1. Lamos EM, Younk LM, Davis SN: Canagliflozin , an inhibitor of sodium-glucose cotransporter 2, for the treatment of type 2 diabetes mellitus. Expert Opin Drug Metab Toxicol. 2013 Jun;9(6):763-75. doi: 10.1517/17425255.2013.791282. Epub 2013 Apr 17. [Article]
  2. Osaki A, Okada S, Saito T, Yamada E, Ono K, Niijima Y, Hoshi H, Yamada M: Renal threshold for glucose reabsorption predicts diabetes improvement by sodium-glucose cotransporter 2 inhibitor therapy. J Diabetes Investig. 2016 Sep;7(5):751-4. doi: 10.1111/jdi.12473. Epub 2016 Feb 16. [Article]
  3. Deeks ED, Scheen AJ: Canagliflozin: A Review in Type 2 Diabetes. Drugs. 2017 Sep;77(14):1577-1592. doi: 10.1007/s40265-017-0801-6. [Article]
  4. Joseph JJ, Golden SH: Type 2 diabetes and cardiovascular disease: what next? Curr Opin Endocrinol Diabetes Obes. 2014 Apr;21(2):109-20. doi: 10.1097/MED.0000000000000044. [Article]
  5. Gleissner CA, Galkina E, Nadler JL, Ley K: Mechanisms by which diabetes increases cardiovascular disease. Drug Discov Today Dis Mech. 2007;4(3):131-140. doi: 10.1016/j.ddmec.2007.12.005. [Article]
  6. Mannucci E, Dicembrini I, Lauria A, Pozzilli P: Is glucose control important for prevention of cardiovascular disease in diabetes? Diabetes Care. 2013 Aug;36 Suppl 2:S259-63. doi: 10.2337/dcS13-2018. [Article]
  7. Steven L. Cowart and Max E. Stachura (1990). Clinical Methods: The History, Physical, and Laboratory Examinations. 3rd edition. (3rd ed.). Butterworths.
  8. U.S. FDA Approves INVOKANA® (canagliflozin) to Reduce the Risk of Heart Attack, Stroke or Cardiovascular Death in Adults with Type 2 Diabetes and Established Cardiovascular Disease [Link]
  9. Diabetes, Heart Disease, and Stroke: NIDDK [Link]
  10. FDA Approved Drug Products: Invokana (canagliflozin) oral tablets [Link]
  11. FDA Approved Products: INVOKAMET (canagliflozin and metformin hydrochloride tablets), for oral use [Link]
  12. FDA Approved Drug Products: Invokana (canagliflozin) tablets for oral use (July 2023) [Link]
  13. Invokana, Canadian monograph [File]
KEGG Drug
D09592
PubChem Compound
24812758
PubChem Substance
175427146
ChemSpider
26333259
BindingDB
50386885
RxNav
1373458
ChEBI
73274
ChEMBL
CHEMBL2048484
ZINC
ZINC000043207238
PDBe Ligand
L3R
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Canagliflozin
PDB Entries
8hdh
FDA label
Download (687 KB)
MSDS
Download (24.7 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentCoronavirus Disease 2019 (COVID‑19)1
4Active Not RecruitingTreatmentType 2 Diabetes Mellitus2
4CompletedTreatmentAlbuminuria / Type 2 Diabetes Mellitus1
4CompletedTreatmentDiabetes Mellitus1
4CompletedTreatmentHearth Failure With Reduced Ejection Fraction (HFrEF) / Type 2 Diabetes Mellitus1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
TabletOral
Tablet, film coatedOral
Tablet, extended releaseOral
Tablet, film coated, extended releaseOral
TabletOral100 mg
TabletOral300 mg
TabletOral300.000 mg
Tablet, film coatedOral100 mg/1
Tablet, film coatedOral300 mg/1
Tablet, film coatedOral
Tablet, film coatedOral100 mg
Tablet, film coatedOral300 mg
Tablet, coatedOral
Tablet, film coatedOral150.00 mg
Tablet, film coatedOral50.00 mg
Tablet, coatedOral100 mg
Tablet, coatedOral300 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US6723340No2004-04-202021-10-25US flag
US8222219No2012-07-172024-07-30US flag
US8513202No2013-08-202027-12-03US flag
US7943582No2011-05-172029-02-26US flag
US8785403No2014-07-222024-07-30US flag
US7943788No2011-05-172027-07-14US flag
US10617668No2020-04-142031-05-11US flag
US11576894No2010-07-062030-07-06US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)68-72https://www.trc-canada.com/product-detail/?CatNum=C175190
boiling point (°C) ‎642.9±55.0http://www.chemspider.com/Chemical-Structure.26333259.html
water solubilityalmost insolublehttps://www.ema.europa.eu/en/documents/assessment-report/invokana-epar-public-assessment-report_en.pdf
logP3.44https://www.tga.gov.au/file/824/download
pKa13.34https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL2103841/
Predicted Properties
PropertyValueSource
Water Solubility0.0045 mg/mLALOGPS
logP3.09ALOGPS
logP3.52Chemaxon
logS-5ALOGPS
pKa (Strongest Acidic)12.57Chemaxon
pKa (Strongest Basic)-3Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count5Chemaxon
Hydrogen Donor Count4Chemaxon
Polar Surface Area90.15 Å2Chemaxon
Rotatable Bond Count5Chemaxon
Refractivity116.14 m3·mol-1Chemaxon
Polarizability46.64 Å3Chemaxon
Number of Rings4Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9541
Blood Brain Barrier+0.7708
Caco-2 permeable-0.6554
P-glycoprotein substrateSubstrate0.6058
P-glycoprotein inhibitor INon-inhibitor0.8414
P-glycoprotein inhibitor IINon-inhibitor0.9447
Renal organic cation transporterNon-inhibitor0.8544
CYP450 2C9 substrateNon-substrate0.6853
CYP450 2D6 substrateNon-substrate0.8293
CYP450 3A4 substrateNon-substrate0.5929
CYP450 1A2 substrateNon-inhibitor0.6579
CYP450 2C9 inhibitorNon-inhibitor0.6178
CYP450 2D6 inhibitorNon-inhibitor0.8683
CYP450 2C19 inhibitorNon-inhibitor0.5958
CYP450 3A4 inhibitorNon-inhibitor0.7086
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7691
Ames testNon AMES toxic0.584
CarcinogenicityNon-carcinogens0.9103
BiodegradationNot ready biodegradable0.9936
Rat acute toxicity2.5975 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9912
hERG inhibition (predictor II)Non-inhibitor0.7246
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-0002-0110900000-6c638b8cc9b7c8253bc1
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-05fr-0010900000-780b01732bb78212c604
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-0059-0293500000-971fac7697402f469e04
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0a4l-6329400000-05216d0f205e9b7873c0
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-01pk-1195400000-ed127b8052948e8ac04c
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-0a4l-4349000000-4f678932f3ddaddb0cdb
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-200.55614
predicted
DeepCCS 1.0 (2019)
[M+H]+202.45152
predicted
DeepCCS 1.0 (2019)
[M+Na]+208.35258
predicted
DeepCCS 1.0 (2019)

Targets

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Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.
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Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Low-affinity glucose:sodium symporter activity
Specific Function
Sodium-dependent glucose transporter. Has a Na(+) to glucose coupling ratio of 1:1.Efficient substrate transport in mammalian kidney is provided by the concerted action of a low affinity high capac...
Gene Name
SLC5A2
Uniprot ID
P31639
Uniprot Name
Sodium/glucose cotransporter 2
Molecular Weight
72895.995 Da
References
  1. Lamos EM, Younk LM, Davis SN: Canagliflozin , an inhibitor of sodium-glucose cotransporter 2, for the treatment of type 2 diabetes mellitus. Expert Opin Drug Metab Toxicol. 2013 Jun;9(6):763-75. doi: 10.1517/17425255.2013.791282. Epub 2013 Apr 17. [Article]
  2. FDA label, Invokana [File]
  3. Invokana, Canadian monograph [File]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Retinoic acid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform has specificity for phenols. Isoform 2 lacks trans...
Gene Name
UGT1A9
Uniprot ID
O60656
Uniprot Name
UDP-glucuronosyltransferase 1-9
Molecular Weight
59940.495 Da
References
  1. Sarnoski-Brocavich S, Hilas O: Canagliflozin (invokana), a novel oral agent for type-2 diabetes. P T. 2013 Nov;38(11):656-66. [Article]
  2. Devineni D, Vaccaro N, Murphy J, Curtin C, Mamidi RN, Weiner S, Wang SS, Ariyawansa J, Stieltjes H, Wajs E, Di Prospero NA, Rothenberg P: Effects of rifampin, cyclosporine A, and probenecid on the pharmacokinetic profile of canagliflozin, a sodium glucose co-transporter 2 inhibitor, in healthy participants. Int J Clin Pharmacol Ther. 2015 Feb;53(2):115-28. doi: 10.5414/CP202158. [Article]
  3. FDA label, Invokana [File]
  4. Invokana, Canadian monograph [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Glucuronosyltransferase activity
Specific Function
UDPGTs are of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isozyme is active on polyhydroxylated estrogens (such as...
Gene Name
UGT2B4
Uniprot ID
P06133
Uniprot Name
UDP-glucuronosyltransferase 2B4
Molecular Weight
60512.035 Da
References
  1. Sarnoski-Brocavich S, Hilas O: Canagliflozin (invokana), a novel oral agent for type-2 diabetes. P T. 2013 Nov;38(11):656-66. [Article]
  2. Devineni D, Vaccaro N, Murphy J, Curtin C, Mamidi RN, Weiner S, Wang SS, Ariyawansa J, Stieltjes H, Wajs E, Di Prospero NA, Rothenberg P: Effects of rifampin, cyclosporine A, and probenecid on the pharmacokinetic profile of canagliflozin, a sodium glucose co-transporter 2 inhibitor, in healthy participants. Int J Clin Pharmacol Ther. 2015 Feb;53(2):115-28. doi: 10.5414/CP202158. [Article]
  3. FDA label, Invokana [File]
  4. Invokana, Canadian monograph [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Mosley JF 2nd, Smith L, Everton E, Fellner C: Sodium-Glucose Linked Transporter 2 (SGLT2) Inhibitors in the Management Of Type-2 Diabetes: A Drug Class Overview. P T. 2015 Jul;40(7):451-62. [Article]
  2. FDA label, Invokana [File]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Not Available
Specific Function
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...
Gene Name
ORM1
Uniprot ID
P02763
Uniprot Name
Alpha-1-acid glycoprotein 1
Molecular Weight
23511.38 Da
References
  1. Lamos EM, Younk LM, Davis SN: Canagliflozin , an inhibitor of sodium-glucose cotransporter 2, for the treatment of type 2 diabetes mellitus. Expert Opin Drug Metab Toxicol. 2013 Jun;9(6):763-75. doi: 10.1517/17425255.2013.791282. Epub 2013 Apr 17. [Article]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Mamidi RNVS, Dallas S, Sensenhauser C, Lim HK, Scheers E, Verboven P, Cuyckens F, Leclercq L, Evans DC, Kelley MF, Johnson MD, Snoeys J: In vitro and physiologically-based pharmacokinetic based assessment of drug-drug interaction potential of canagliflozin. Br J Clin Pharmacol. 2017 May;83(5):1082-1096. doi: 10.1111/bcp.13186. Epub 2016 Dec 20. [Article]
  2. Devineni D, Vaccaro N, Murphy J, Curtin C, Mamidi RN, Weiner S, Wang SS, Ariyawansa J, Stieltjes H, Wajs E, Di Prospero NA, Rothenberg P: Effects of rifampin, cyclosporine A, and probenecid on the pharmacokinetic profile of canagliflozin, a sodium glucose co-transporter 2 inhibitor, in healthy participants. Int J Clin Pharmacol Ther. 2015 Feb;53(2):115-28. doi: 10.5414/CP202158. [Article]
  3. FDA label, Invokana [File]
  4. Invokana, Canadian monograph [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Organic anion transmembrane transporter activity
Specific Function
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name
ABCC2
Uniprot ID
Q92887
Uniprot Name
Canalicular multispecific organic anion transporter 1
Molecular Weight
174205.64 Da
References
  1. Invokana, Canadian monograph [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
References
  1. Invokana, Canadian monograph [File]

Drug created at June 17, 2013 06:21 / Updated at March 18, 2024 16:48